Back to Journals » International Journal of Nanomedicine » Volume 11

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Authors Ahmed T

Received 11 October 2015

Accepted for publication 23 December 2015

Published 2 February 2016 Volume 2016:11 Pages 515—527


Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Farooq Shiekh

Peer reviewer comments 5

Editor who approved publication: Dr Thomas J Webster

Tarek A Ahmed1,2

1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

Abstract: In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability.

Keywords: finasteride, nanoparticles, solvent evaporation, optimization, crystal growth, pharmacokinetic

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]


Readers of this article also read:

Liquid crystal nanoparticle formulation as an oral drug delivery system for liver-specific distribution

Lee DR, Park JS, Bae IH, Lee Y, Kim BM

International Journal of Nanomedicine 2016, 11:853-871

Published Date: 3 March 2016

Pigment epithelial-derived factor gene loaded novel COOH-PEG-PLGA-COOH nanoparticles promoted tumor suppression by systemic administration

Yu T, Xu B, He L, Xia S, Chen Y, Zeng J, Liu Y, Li S, Tan X, Ren K, Yao S, Song X

International Journal of Nanomedicine 2016, 11:743-759

Published Date: 25 February 2016

Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers

Lim CM, Youn YS, Lee KS, Hoang NH, Sim TH, Lee ES, Oh KT

International Journal of Nanomedicine 2016, 11:703-713

Published Date: 22 February 2016

Toward a general physiologically-based pharmacokinetic model for intravenously injected nanoparticles

Carlander U, Li D, Jolliet O, Emond C, Johanson G

International Journal of Nanomedicine 2016, 11:625-640

Published Date: 11 February 2016

Efficient inhibition of ovarian cancer by degradable nanoparticle-delivered survivin T34A gene

Luo L, Du T, Zhang J, Zhao W, Cheng H, Yang Y, Wu Y, Wang C, Men K, Gou M

International Journal of Nanomedicine 2016, 11:501-513

Published Date: 2 February 2016

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Yousaf AM, Mustapha O, Kim DW, Kim DS, Kim KS, Jin SG, Yong CS, Youn YS, Oh YK, Kim JO, Choi HG

International Journal of Nanomedicine 2016, 11:213-221

Published Date: 12 January 2016

Dendrimers as tunable vectors of drug delivery systems and biomedical and ocular applications

Kalomiraki M, Thermos K, Chaniotakis NA

International Journal of Nanomedicine 2016, 11:1-12

Published Date: 22 December 2015